Nelfinavir Metabolization (HIV)
Nelfinavir is an antiretroviral drug used in the treatment of patients with HIV infection.
Nelfinavir binds irreversibly to the active part of the HIV protease, thereby preventing the division of viral precursor polyproteins, forming immature, non-infectious viral particles.
Hypersensitivity to the active substance or to any of the excipients.
The concomitant administration of nelfinavir with the following drugs is contraindicated: rifampicin, ergot derivatives, cisapride, pimozide, oral midazolam, triazolam, St. John's wort, simvastatin, lovastatin and sildenafil in the treatment of pulmonary hypertension.
An increase in spontaneous bleeding has been reported in hemophiliacs.
In patients with hepatic insufficiency it has been described elevation of liver transaminases, higher risk in patients infected with HBV or HCV.
Like other HIV protease inhibitors, the use of nelfinavir has been associated to the appearance of dyslipidemia, redistribution of body fat, nephrolithiasis and diabetes, especially in the long term.
The most frequent adverse effects are diarrhea, leukopenia, neutropenia, skin rash, anorexia and abdominal pain.
Nelfinavir is metabolized in part by CYP34A4 cytochrome and is a substrate of CYP2C19 and CYP3A4, so it is expected to produce numerous drug interactions.
Unlike other protease inhibitors, potentiation with ritonavir does not significantly increase nelfinavir concentrations, so ritonavir administration is not recommended.
It is recommended to administer nelfinavir with acution when administering together with the following groups of drugs: other antiretroviral drugs, oral anticoagulants, antiepileptics (phenytoin, carbamazepine, phenobarbital), azole antifungals, macrolide antibiotics, immunosuppressants (cyclosporine, tacrolimus, sirolimus), antiarrhythmics (quinidine, propafenone, amiodarone , lidocaine, digoxin).
In any case, close monitoring of the therapeutic efficacy and toxicity of nelfinavir and concomitant treatments is recommended
- Viracept ®
Gene or region studied